2. Academic Validation
  3. Developing a Gadolinium(III) Compound Based on Apoferritin for Targeted Magnetic Resonance Imaging and Dual-Modal Therapy of Cancer

Developing a Gadolinium(III) Compound Based on Apoferritin for Targeted Magnetic Resonance Imaging and Dual-Modal Therapy of Cancer

  • J Med Chem. 2023 May 22. doi: 10.1021/acs.jmedchem.2c01904.
Xueyu Man 1 2,  Tongfu Yang 1,  Wenjuan Li 1,  Shanhe Li 1,  Gang Xu 1,  Zhenlei Zhang 1,  Hong Liang 1,  Feng Yang 1
Affiliations

Affiliations

  • 1 State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources/Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Ministry of Education of China), School of Chemistry and Pharmaceutical Sciences, Collaborative Innovation Center for Guangxi Ethnic Medicine, Guangxi Normal University, Guilin, Guangxi 541004, China.
  • 2 School of Pharmacy, Zunyi Medical University, Zunyi, Guizhou 563006, China.
PMID: 37218052 DOI: 10.1021/acs.jmedchem.2c01904
Abstract

To integrate targeted diagnosis and treatment of Cancer, we proposed to develop a gadolinium (Gd) agent based on the properties of apoferritin (AFt). To this end, we not only optimized a series of Gd(III) 8-hydroxyquinoline-2-carboxaldehyde-thiosemicarbazone compounds to obtain a Gd(III) compound (C4) with remarkable T1-weighted magnetic resonance imaging (MRI) performance and cytotoxicity to Cancer cells in vitro but also constructed an AFt-C4 nanoparticle (NP) delivery system. Importantly, AFt-C4 NPs improved the targeting ability of C4 in vivo and showed enhanced MRI performance and tumor growth inhibition ratio relative to C4 alone. Furthermore, we confirmed that C4 and AFt-C4 NPs inhibited tumor growth through Apoptosis, Ferroptosis, and ferroptosis-induced immune response.

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